Bench-Stable Transfer Reagent Facilitates the Generation of Trifluoromethyl-sulfonimidamides,The Journal of Organic Chemistry

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Bench-Stable Transfer Reagent Facilitates the Generation of Trifluoromethyl-sulfonimidamides
The Journal of Organic Chemistry ( IF 3.3 ) Pub Date : 2018-06-22 00:00:00 , DOI: 10.1021/acs.joc.8b01244
Miranda Wright ₁ , Carolina Martínez-Lamenca ₂ , Joseph E. Leenaerts ₂ , Paul E. Brennan ₁ , Andrés A. Trabanco ₃ , Daniel Oehlrich ₂

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Sulfonimidamides are an emerging bioisosteric replacement in medicinal chemistry projects, and therefore new chemistries are necessary to access this functionality. The general synthesis of CF₃-sulfonimidamides from an activated bench-stable transfer reagent is described. A diverse reaction scope is demonstrated, with a wide range of nucleophilic amines being tolerated in this transformation. The CF₃-sulfonimidamides obtained contain an additional diversity point, in the form a protected imine, that could be unmasked to allow late stage modifications.

中文翻译：

稳定的转移试剂有助于生成三氟甲基亚磺酰胺

磺酰胺类药物是药物化学项目中正在出现的生物等位替代物，因此，使用新的化学方法以使用该功能是必要的。描述了由活化的台式稳定的转移试剂合成CF _3-磺酰亚胺酰胺的一般方法。证明了多样化的反应范围，在该转化中可耐受多种亲核胺。所获得的CF _3-亚磺酰胺酰胺包含额外的多样性点，其形式为受保护的亚胺，可以暴露出来以允许后期修饰。

更新日期：2018-06-22

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